opiates and opioids Flashcards

You may prefer our related Brainscape-certified flashcards:
1
Q

what is an opiate?

A

natural narcotic opioid found in the opium poppy (papaver somniferum)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

what is an opioid?

A

any natural or synthetic compound or endogenous peptides that exert biological effects at the opioid receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

what are the 3 major psychoactive opiates

A

major- morphine, codeine, thebaine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

what are the three pharmacological use of natural opiates and which one is known to be the most potent and effective pain reliever

A

analgesic, antitussive, and decreased gastric motility

analgesic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

what does antitussive and decreased gastric motility do

A

antitussive-> cough suppressant, in which codeine has decreased the analgesic effect but retains antitussive effects

decreased gastric motility-> can be used to treat diarrhea esp pathogenic
-> Loperamide is an opioid derivative that does not penetrate the BBB and is used to treat diarrhea

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

what is an example of semi-synthetic opioid, what was the trade name that it was under and what was it used for

A

diacetylmorphine
heroin
cough suppressant, analgesic, and cure for morphine addiction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

what are the administration routes for natural opiates

A

oral- morphine readily absorbed through GI but high variability, codeine has more consistent oral absorption

Subcutaneous, IM, IV- more stable systematic levels and IM is the preferred routes for morphine in clinical setting and IV is common for recreational use

inhalation- historic route of (recreational) administration for raw opium is smoking

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

what are the administration routes for semi-synthetic opioid?

A

oral- heroin administration by oral route produces the same potency and efficacy as morphine

IV- dramatically more potent and rapid than morphine due to increased lipophilic structure (increased BBB permeability)

inhalation or intranasal-> occasional route for recreational use

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Fill in the blank: Development of numerous semi-synthetic opioids followed the isolation of ________ and _______ and subsequent discovery of the structures

A

morphine and codeine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

TRUE OR FALSE: freebase heroin can be smoked while other preparations can be finely ground and snorted

A

true

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

at what doses do opioids exert limited psychoactive effects

A

5-10mg morphine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

what are 5 therapeutic effects of opioids?

A

pain relief, drowsiness, constriction of pupils, decreased sensitivity to external or internal stimuli, dream-filled sleep

for more, look at slide 10

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

what are two subjective effects of high doses of opioids

A

-euphoria or elation ( in contrast to relaxed state at lower doses)
- rush-> most pronounced by IV (rapid, intense state of euphoria, described by others as a “whole body orgasm”)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

what are three physiological effects of high doses?

A

pinprick pupils, nausea and vomiting ( opioids can act at the chemoreceptor trigger zone in the area postrema to induce the vomit reflex) and moderate respiratory depression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Fill in the blank: Prescription opioids (________) are one of the fastest growing classes of drugs of abuse

A

oxycontin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

TRUE OR FALSE: tolerance to opioids develops slowly and tolerance to respiratory and euphoric effects develops more slowly than tolerance to analgesic effects

A

false: quickly and rapidly

14
Q

what are the 3 types of tolerance?

A

metabolic-> some increase in drug metabolism
behavioural-> highly relevant in addicts
pharmacodynamic-> principle mechanism of tolerance– decreased expression of opioid receptors

15
Q

what is the reason why there are somewhat exaggerated perceptions of opioid withdrawal

A

cinematic creative license

16
Q

True or false: opioid withdrawals are much more severe than withdrawal from barbiturates or alcohol

A

false; much less severe, since severe alcohol withdrawal can be fatal

opioids never fatal

17
Q

what two things is withdrawal heavily influenced by

A

drug tolerance and dependence (check slide 15 for extra information and graph)

18
Q

what is rebound hyperactivity?

A

withdrawal produces neurochemical and behavioural changes that are often opposite to the effects of intoxication

19
Q

when do stages of withdrawal begin

A

6-12 hours after last administration, peaks 26-27hours persists less than 1 week

20
Q

what can be seen in the first stage of withdrawal

A
  • Restlessness and agitation is first sign
  • Excess yawning, agitation, violence
  • Chills, hot flashes, shortness of breath
  • Intense piloerection (goosebumps) – origin of the term ‘cold turkey’
  • Increasing drowsiness and deep sleep (often 8-12 hours)
21
Q

what can be seen in the second stage of withdrawal

A
  • Cramps in stomach, back, legs
  • Vomiting, diarrhea, profuse sweating
  • Twitching of the extremities – shaking of hands and kicking of legs – origin of the term ‘kicking the habit’
  • Symptoms become progressively less severe until gradually disappearing
22
Q

what is withdrawal symptoms reduced by and what stop withdrawal immediately

A
  • reduced by alcohol
  • stopped immediately by opioid administration which is induced by opioid antagonists
23
Q

what kind of administration of high doses cause death

A

IV heroin or morphine

24
Q

what are some of the results from high doses of opioids (overdose)

A
  • Comatose state, pinpoint pupils, and severe respiratory depression
  • Lowers seizure threshold – convulsions common
  • Death occurs by severe respiratory depression or combination of supressed cough reflex, unconsciousness, and vomiting
  • Contaminants such as quinine (used to cut heroin) are a probable cause of many overdoses – causes frothing from mouth and nose and death by pulmonary edema
25
Q

what is opioid overdose affected by

A

behavioural tolerance- drug use outside conditioned environment can lead to increased drug effects

26
Q

what can be used to treat an overdose

A

opioid antagonists (naloxone)

27
Q

what is a major side effect of clinical opioid use which does not develop tolerance?

A

constipation

28
Q

what are two other chronic effects of opioid use

A
  • Hormone imbalance
    ->Hypogonadism in majority of chronic opioid
    users (up to 90%)
    ->Amenorrhea by supressing luteinizing
    hormone
  • Opioid-induced hyperalgesia (remember this, it is the most important one)
    ->Chronic opioid use alters the homeostasis
    of pain signalling pathways
    ->With time pain thresholds decrease resulting
    in increased sensitivity to pain – often
    mistaken for tolerance resulting in increased
    dosage
29
Q

what are two ways to manage addictions

A

maintenance therapies- the real harm of opioid abuse is caused by illegality and expense of the drug
british system- provides heroin prescription to addicts at public expense

30
Q

why is there a large amount of adverse health effects of opioid abuse

A

due to the impurities in drug and spread of diseases (HIV, hepatitis) due to unsafe administration

31
Q

what is methadone maintenance (the US system)

A
  • Synthetic opioid administered orally
  • Decreased euphoric effects
  • Effects last ~24 hours in preventing withdrawal symptoms
  • Competitive for receptor sites with morphine (blocks euphoric effects of heroin if co-administered)
  • Reduces associated morbidity and mortality
  • 80-90 % relapse rates
32
Q

True or false: methadone has increased potency and increased effects and only has a short duration of effect

A

false; decrease, decrease, longer duration of effect

33
Q

true or false: methadone withdrawal is much less severe than heroin

A

true

34
Q

what is LAMM

A
  • Orally administrable maintenance drug
  • Comparable to methadone therapy but longer lasting – up to 72 hours (administration required only 3x per week)
  • Some risk of life-threatening ventricular rhythm disorders (not widely used)
35
Q

what is buprenorphine

A
  • Analgesic, mixed agonist-antagonist at different opioid receptors
  • Similar to methadone, but fewer adverse effects (no respiratory depression)
  • Is itself addictive, but thought to be easier to kick than heroin
  • Investigational use in neonatal abstinence – infants born to opioid addicted mothers
  • Suboxone is currently favoured in Canada – buprenorphine and naloxone